Insulin Secretagogues Flashcards
Insulin Secretagogues cause what to occur?
Insulin to be secreted from beta cells in the pancreas
Describe the regulation cascade for insulin to be secreted?
(+) Gs GPCR
- AC
- cAMP
- PKA
- Calcium current opened more to allow it in the cell
- Insulin leaves cell
Which GPCR (-) the release of insulin by (-) the regulation cascade?
Gi
What 2 things can (+) Gs GPCR to increase insulin secretion from the cell?
GLP-1 Agonists
Beta 2 Agonists
What 2 things can (-) insulin secretion by (+) Gi GPCR?
Alpha 2 agonists
Somatostatin
What are the 2 classes of Incretin Mimetics?
GLP-1 Agonists
DPP-4 Inhibitors
What are the 2 GLP-1 Agonists?
Exenatide
Liraglutide
What are the 2 GLP-1 Agonists?
Exenatide
Liraglutide
What is the MOA for GLP-1 Agonists?
(+) Gs GPCR - AC - cAMP - PKA - Calcium influx = Insulin release
Which GLP-1 Agonist has the shorter half life?
Exenatide
Which GLP-1 Agonist is bound to Albumin?
Liraglutide
When are GLP-1 Agonists used?
Type 2 DM that is not well controlled when the patient is already on other meds
Compared to other insulin secretagogues, how does the hypoglycemia risk compare with GLP-1 Agonists?
LOWER risk
Normal Action of Incretins like GLP-1?
(+) insulin
(-) Glucagon
= Lower blood glucose postprandially
How are GLP-1 Agonists and DPP-4 Inhibitors given?
GLP-1 Agonists = parenteral
DPP-4 Inhibitors = oral
What is the normal job of DPP-4?
(-) GLP-1
= Increases blood glucose because insulin is not activated/glucagon not suppressed
What are the DPP-4 Inhibitors?
- GLIPTINS
What are the DPP-4 Inhibitors?
-GLIPTINS
What 2 classes of drugs can block the K+ channel to increase insulin release?
Sulfonylureas
Meglitinides
The 1st Gen Sulfonylureas are rarely used. What are they?
- AMIDES
What are the 1st Gen Sulfonylureas?
- AMIDES
Why are the 2nd Gen Sulfonylureas better?
Higher potency and LESS adverse effects
What are the 2nd Gen Sulfonylureas?
GLI/Y ____
What are the 2nd Gen Sulfonylureas?
GLY/I _____
